US5322951AExpiredUtilityPatentIndex 72
Certain 1-(2,3-dihydro-indole)carbonyl intermediates
Est. expiryJan 5, 2007(expired)· nominal 20-yr term from priority
C07D 451/04
72
PatentIndex Score
13
Cited by
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References
2
Claims
Abstract
An intermediate compound of Formula (V): ##STR1## wherein G is COQ 1 and Q 1 represents chloro, bromo, C 1-4 alkoxy, PhO--, Cl 5 C 6 O--, Cl 3 CO--, succinimidyloxy or imidazolyloxy; the remainder of the terms R 1 , R 2 , R 3 , R 4 , X and Y are defined in the specification. The intermediates of Formula V are useful for preparing 1-(2,3-dihydro-1-carboxamide final products wherein said final products possess 5-HT M-receptor antagonist activity.
Claims
exact text as granted — not AI-modifiedWe claim:
1. An intermediate compound of formula (V): ##STR57## wherein G is COQ 1 wherein Q 1 is Chloro, bromo, C 1-4 akoxy, PhO--, Cl 5 C 6 O--, Cl 3 CO--, succinimidyloxy or imidazolyloxy; X and Y are independently selected from hydrogen or C 1-4 alkyl, or together are a bond; R 1 and R 2 are independently selected from hydrogen, C 1-6 alkyl, C 2-6 alkenyl-C 1-4 -alkyl, or together are C 2-4 polymethylene; and R 3 and R 4 are independently selected from hydrogen, halogen, CF 3 , C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkylthio, C 1-7 -acyl, C 1-7 acylamino, C 1-6 alkylsulphonylamino, N-(C 1-6 alkylsulphonyl)-N-C 1-4 -alkylamino, C 1-6 -alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or Np(aminosulphonyl)-C 1-4 alkylamino optionally N-substituted by one or two groups selected from C 1-6 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl C 1-4 alkyl, phenyl or phenyl C 1-4 alkyl groups or optionally N-disubstituted by C 4-5 polymethylene.
2. An intermediate compound selected from the group consisting of: 1-(2,3-dihydro)-indolyltrichloromethyl carbamate, 1-(2,3-dihydro-3-methyl)indolyl-O-(1-succinimidyl)carbamate, 1-(2,3-dihydro-5-fluoro)indolyl-O-(1-succinimidyl)carbamate, 1-(2,3-dihydro-5-methoxy)indolyl trichloromethyl carbamate, 1-(2,3-dihydro)-indolylcarbonyl chloride, 1-(2,3-dihydro-3-ethyl)indolylcarbonyl chloride, 1-(2,3-dihydro-5-nitro)indolyl-trichloromethyl carbamate, 1-[1-(2,3-dihydro-6-nitro)indolylcarbonyl]-imidazole, and 1-(2,3-dihydro-3,3-dimethyl)indolylcarbonyl chloride.Cited by (0)
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